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CCF642 

Cat. No.: HY-100430 Purity: >98.0%
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CCF642 is a potent protein disulfide isomerases (PDI) inhibitor with an IC50 of 2.9 μM. CCF642 causes acute endoplasmic reticulum (ER) stress in multiple myeloma cells accompanied by apoptosis-inducing calcium release. CCF642 has broad anti-multiple myeloma activity.

For research use only. We do not sell to patients.

CCF642 Chemical Structure

CCF642 Chemical Structure

CAS No. : 346640-08-2

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10 mM * 1 mL in DMSO USD 75 In-stock
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100 mg USD 650 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

CCF642 is a potent protein disulfide isomerases (PDI) inhibitor with an IC50 of 2.9 μM. CCF642 causes acute endoplasmic reticulum (ER) stress in multiple myeloma cells accompanied by apoptosis-inducing calcium release. CCF642 has broad anti-multiple myeloma activity[1].

IC50 & Target

IC50: 2.9 μM (PDI)[1]

In Vitro

CCF642 (3 μM; 0.5-6 hours) increases PERK dimerization by phosphorylation and IRE1-α oligomerization within 30 minutes in KMS-12-PE confirming accumulation of misfolded ER proteins[1].
CCF642, a bone marrow-sparing compound, exhibits a submicromolar IC50 in 10 of 10 multiple myeloma cell lines (MM1.S, MM1.R, KMS-12-PE, KMS-12-BM, NCI-H929, U266, RPMI 8226, JJN-3, HRMM.09-luc, 5TGM1-luc)[1].

Western Blot Analysis[1]

Cell Line: MM1.S cells
Concentration: 3 μM
Incubation Time: 0.5, 1, 2, 4, 6 hours
Result: Increased PERK dimerization by phosphorylation and IRE1-α oligomerization within 30 minutes in KMS-12-PE confirming accumulation of misfolded ER proteins.
In Vivo

CCF642 (10 mg/kg; i.p.; three times a week; for 24 days) significantly prolongs life of 5TGM1-luc-bearing mice and suppresses 5TGM1-luc growth as determined by life imaging[1].

Animal Model: C57BL/KaLwRij mice of 6 to 8 weeks of age with 5TGM1-luc[1]
Dosage: 10 mg/kg
Administration: i.p.; three times a week; for 24 days
Result: Significantly prolonged life of 5TGM1-luc–bearing mice and suppressed 5TGM1-luc growth as determined by life imaging.
Molecular Weight

378.45

Formula

C₁₅H₁₀N₂O₄S₃

CAS No.

346640-08-2

SMILES

O=C1N(C2=CC=C(OC)C=C2)C(S/C1=C/C3=CC=C([N+]([O-])=O)S3)=S

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 30 mg/mL (79.27 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6424 mL 13.2118 mL 26.4236 mL
5 mM 0.5285 mL 2.6424 mL 5.2847 mL
10 mM 0.2642 mL 1.3212 mL 2.6424 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 0.62 mg/mL (1.64 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References
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Keywords:

CCF642CCF 642CCF-642OthersproteindisulfideisomerasesPDIERstressmultiplemyelomaapoptosiscalciumreleaseanti-multipleInhibitorinhibitorinhibit

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CCF642
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HY-100430
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